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Pharm Block 5 > Drugs used in coagulation and blood disorders > Flashcards

Drugs used in coagulation and blood disorders Flashcards

1
Q

What are the activators of clot formation?

A

ADP, Thromboxane and serotonin

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2
Q

What clotting factors are inhibited by heparin?

A

9a, 10a, 11a

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3
Q

What clotting factors are inhibited by warfarin?

A

2,7,9,10, Protein C & S

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4
Q

What is the mechanism of heparin?

A

Heparin binds antithrombin III to inactivate thrombin (IIa), which blocks formation of fibrin immediately

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5
Q

What are the low molecular weight heparins?

A

Enoxaprin, Dalteparin, and Tinzaparin

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6
Q

What is the antidote for heparin overdose?

A

Protamine sulfate is a positively charged protein neutralizes heparin electrically. Adverse effects are coagulation, drop in BP, hypersensitivity.

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7
Q

What is the mechanism of the low molecular weight heparin?

A

accelerates antithrombin III activity, inactivating factor Xa and IIa (thrombin)

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8
Q

What is fondaparinix?

A

a synthetic pentasaccharide that bind antithrombin and enhances inactivation of Xa. Inhibits thrombin but doesn’t act on thrombin specifically. aPTT not a good measurement

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9
Q

What is the Glysoaminoglycans that are available outside the US?

A

Danaparoid, selective for thrombin

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10
Q

How is the action of heparin monitored?

A

aPTT laboratory test (activated partial thromboplastin time)

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11
Q

Which anticoagulant is safe in pregnancy?

A

heparin

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12
Q

What are the direct thrombin inhibitors? Which ones are available orally?

A

Lipirudin, Bivalirudin, Argatroban, Dabigatran. Dabigatran is available orally, the rest are available parenterally.

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13
Q

What is the mechanism of the direct thrombin inhibitors?

A

bind and inactive thrombin

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14
Q

What are direct thrombin inhibitors used?

A

DVT, pulmonary embolism, prophylaxis during elective surgery, acute phase of MI, DIC

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15
Q

What do you give to patients in heparin-induced thrombocytopenia?

A

Lipirudin

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16
Q

When do you get hypersensitivity reactions?

A

Typically only with unfractioned heparin.

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17
Q

What is the antidote for the parenteral (non-heparin) anticoagulants?

A

fresh frozen plasma which contains Xa, IIa. No reversing agents exist.

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18
Q

What are the oral anticoagulants

A

Warfarin, Dicumarol, Anisindione

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19
Q

Which drugs can enhance the effects of Warfarin?

A

sulfonamides, 3rd generation cephalosporins, PPIs, anything metabolized through cytochrome P450

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20
Q

What is the mechanism of warfarin, dicumarol, and anisindione?

A

inhibits vit K epoxide reductase, preventing reduced vit K activation of clotthing factors 2, 7,9,10, Protein C and S.

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21
Q

What are the uses of warfarin, diucumarol, and anisindione?

A

chronic anticoagulation after MI, DVT, artificial heart valves.

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22
Q

How long does it take for warfarin to kick in?

A

half life of clotting factors is 8 - 60 hours, so requires all preformed clotting factors to be used up before it kicks in.

23
Q

What do you do while waiting for warfarin to kick in?

A

Tx with heparin for first 3 days.

24
Q

What are adverse effects of oral anticoagulants (warfarin, dicumarol, and anisindione?

A

Rebound hypercoagulable state. Some factors come back rapidly like Protein C (8hr half life).
Bleeding disorders, drug interactions (esp. with PPIs). CI in pregnancy

25
Q

What are the antidotes for Warfarin?

A

Phytonadione (Vit K1), Menadione (Vit K2). These increase Vit K stores in newborns or older patients with abnormal fat absorption. AE are bronchospasm, hypersensitivity, and GI upset.

26
Q

What are the antiplatelet drugs?

A

Aspirin, Ticlopidine, Clopidogrel, Dipyridamole, Glycoprotein IIb/IIIa inhibitors

27
Q

What are the uses of the anti-platelet drugs?

A

prophylactic treatment of transient cerebral ischemia and stroke; reduce incidence of recurrent MI; decrease mortality in post MI

28
Q

What are the adverse effects of antiplatelet drugs?

A

Prolonged bleeding time

29
Q

What is the mechanism of aspirin?

A

Irreversible inhibitor of COX, which reduces thromboxane A2 synthesis and platelet aggregation.

30
Q

When do you treat with Aspirin?

A

heart valve replacement to reduce platelet aggregation; reduce risk of sudden death or MI in patients with angina; reduce risk of strokes.

31
Q

What are AE of aspirin?

A

gastric irritation, prolonged bleeding times

32
Q

What are the ADP-binding inhibitors?

A

Ticlopidine, Clopidogrel

33
Q

What is the mechanism of Ticlopidine and Clopidogrel?

A

inhibits expression of platelet glycoprotein II, III receptors, thus reducing fibrinogen binding and platelet aggregation.

34
Q

What are the adverse effects of Ticlopidine and Clopidogrel?

A

leukopenia, N/V, GI upset

35
Q

What is the mechanism of Dipyridamole?

A

inhibits cyclic nucleotide phosphodiesterase leading to inhibition of thromboxane A2 synthesis. Also decrease adenosine uptake in tx of angina.

36
Q

What is dipyridamole used to treat?

A

prophylaxis of angina, with aspirin use to inhibit embolization from prosthetic heart valves

37
Q

What are the adverse effects of dipyridamole?

A

headache, dizziness

38
Q

What are the Glycoprotein IIb, IIIa receptor inhibitors?

A

Abciximab, Tirofiban, Eptifibatide

39
Q

What is the mechanism of Abciximab, Tirofiban, and Eptifibatide?

A

bind to platelet glycoproteins IIb, IIIa receptors to prevent fibrinogen binding.

40
Q

What are Abciximab, Tirofiban, and Eptifibatide used to tx?

A

prevention of thrombosis in patients undergoing coronary angioplasty.

41
Q

What are common combinations of antiplatelet agents?

A

Aspirin + dipyridamole

Warfarin + dipyridamole

42
Q

What are the thrombolytic agents and how are they given

A

IV: Alteplase/TPA, Reteplace, Anistreplase, Streptokinase, Urokinase

43
Q

Which of the thrombolytic agents is isolated from human urine?

A

Urokinase

44
Q

How do the thombolytic agents work?

A

convert plasminogen to plasmin, which breaks down fibrinogen and fibrin

45
Q

What are the uses of the thrombolytic agents?

A

dissolve existing thrombi in the tx of MI, coronary artery thrombosis, pulmonary embolism, DVT, and occluded access shunts.

46
Q

AE of thrombolytic agents?

A

bleeding complications, hypersensitivity reactions (worst in streptokinase)

47
Q

What is the antidote for thombolytic agents?

A

Aminocaproic acid

48
Q

What drugs are used to treat bleeding disorders?

A

Aminocaproic acid, tranexamic acid, aprotinin

49
Q

What is the mechanism of Aminocaproic acid, tanexeamic acid?

A

inhibit plasminogen activations, thereby inhibiting fibronolysis

50
Q

What are AD of aminocaproic acid and tanexeamic acid?

A

Thomboses (big clots), hypotension, abdominal discomfort

51
Q

What factors do you give patients with hemophilia?

A

VIII and IX, but FFP.

52
Q

What is the risk of giving clotting factors of FFP?

A

infections and immunologic reactions

53
Q

What is cryoprecipitate?

A

FFP with just XIII, VIII, VwF

Pharm Block 5 (9 decks)

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